Cancer has become one of the major global health concerns and remains as the second cause of mortality after cardiovascular diseases. One of the hallmarks of cancer is the uncontrolled cell growth causing more deaths than AIDS, tuberculosis, and malaria combined and one in eight deaths worldwide is due to cancer. As it is caused by both external and internal factors, a balanced approach to cancer control includes prevention, early detection, and effective treatment. In the treatment of cancer, chemotherapy is one of the practical and widely used methods employing drugs that can destroy cancer cells by obstructing their proliferation and reproduction.
The chemotherapeutic drugs include DNA interactive agents, DNA topoisomerase I and II inhibitors, carbonic anhydrase (CA) inhibitors, CDK inhibitors, tubulin polymerization inhibitors, antimitotic agents, anti-metabolites, and miscellaneous agents affecting various cellular processes within the cancer cells. Amongst them, the tubulin binding drugs are one of the successful chemotherapeutic compounds used for cancer treatment. In addition, safety profile and side effects are the major concerns with anticancer drugs. Therefore, the development of novel agents with increased efficacy while reducing the side effects will encourage the researchers towards the drug design and development.
Inhibition of tubulin polymerization is the target of many antitumoural agents known as antimitotic agents or spindle poison and representative examples like colchicines, podophyllotoxins and combretastatins are compounds that inhibit microtubule assembly by binding to tubulin. Many chalcone moieties showed potential biological properties particularly anticancer activity. (Ahcene B., Julien B., Pierre-Alain C., Edwige N., Madeleine B., Annabelle G., Luc C., Denis W., Eva-Laure M., and Charles D., J. Med. Chem. 2008, 51, 2307-2310; Franco C., Rossella F., Francisco O., Francesco O, Stefano A., J. Med. Chem. 2009, 52, 2818-2824; Srinivas K. K.; Erin H.; Catherine P.; Hallur G., Nancy E. D., Saeed R. K.; J. Med. Chem. 2003, 46, 2813-2815; Vineet K.; Sarvesh K.; Mohammad H.; Hailong W.; Rajesh K. T.; Amit K.; Sunil K. S.; Virinder S. P.; Shyam B.; Sanjay V. M. J. Med. Chem. 2011, 54, 4147-4159; Bhat B. A.; Dhar K. L.; Puri S. C.; Saxena A. K.; Shanmugavel M.; Qazi G. N.; Bioorg. Med. Chem. Lett. 2005; 15, 3177-3180).
